The Novel anti-Tumor Agents of 4-Triazol-1,8-naphthalimides: Synthesis, Cytotoxicity, DNA Intercalation and Photocleavage.

Abstract A novel series of 4-(4-phenyl-[1,2,3]-triazol-1-yl)-1,8-naphthalimide derivatives had been synthesized easily by employing “click reaction”. For anti-tumor activity in vitro, all the compounds were found to be more toxic against MCF-7 than Hela and 7721 cells. 4a , 4b and 4e Showed improved cytotoxic activity against MCF-7 cells over Amonafide, in particular compound 4a , with an IC 50 could amount to 10 −7  M. The UV–vis spectra and Circular Dichroism titration indicated that the compounds behaved as effective DNA-intercalating agents. The investigation of their photo-damaging ability illuminated that these compounds could damage DNA effectively into form II and even form III.